PHARM 201 Questions and Verified Answers, 100% Guarantee
When making a drug, what is the easier template to follow? - Easier drug to make is
something that mimics the substrate the enzyme binds to
Covalent Bond
Are these good drugs? - Strongest bond that can be made.
Irreversible.
As drugs, not frequently used because duration of action is too long, not specific and are very
reactive
How does covalent binding occur? - Occurs when a nucleophile (-) attacks an electrophile
(+)
What type of molecule is serine? - Always a nucleophile
Alkylation - A type of covalent drug binding
Occurs when a nucleophile attacks an electrophile
Acylation - A type of covalent drug binding
Occurs when a nucleophile attacks an electrophile.
But only if the groups are: amides, lactones, lactams, ester
(contains COOH or N-C=O)
, Acetylation - A type of acylation (covalent drug binding)
Involves lactones and esters only.
Carbamylation - A type of acylation (covalent drug binding)
Involves lactams and amides only.
Phosphorylation - A type of covalent drug binding
Involves organophosphates and Ach (contains serine)
A irreversible process once the phosphorylation of serine has been aged
If not aged, can administer something to recover ACh
Rearrangement - A type of covalent drug binding. Not common
Involves the metabolic activation of a prodrug to create the reactive metabolite
Pseudo-irreversible acylation - Occurs when the acylation (covalent drug binding) is not
truly irreversible -- original target can be restored over time
Non-covalent bonds - Weaker bonds. Most common in drugs.
Functional groups must be close enough to interact (should have exposed sites)
Ionic Bond - Strongest type of non-covalent bond
Involves ionizable acidic (-) and basic (+)/ quat ammonium functional group
When making a drug, what is the easier template to follow? - Easier drug to make is
something that mimics the substrate the enzyme binds to
Covalent Bond
Are these good drugs? - Strongest bond that can be made.
Irreversible.
As drugs, not frequently used because duration of action is too long, not specific and are very
reactive
How does covalent binding occur? - Occurs when a nucleophile (-) attacks an electrophile
(+)
What type of molecule is serine? - Always a nucleophile
Alkylation - A type of covalent drug binding
Occurs when a nucleophile attacks an electrophile
Acylation - A type of covalent drug binding
Occurs when a nucleophile attacks an electrophile.
But only if the groups are: amides, lactones, lactams, ester
(contains COOH or N-C=O)
, Acetylation - A type of acylation (covalent drug binding)
Involves lactones and esters only.
Carbamylation - A type of acylation (covalent drug binding)
Involves lactams and amides only.
Phosphorylation - A type of covalent drug binding
Involves organophosphates and Ach (contains serine)
A irreversible process once the phosphorylation of serine has been aged
If not aged, can administer something to recover ACh
Rearrangement - A type of covalent drug binding. Not common
Involves the metabolic activation of a prodrug to create the reactive metabolite
Pseudo-irreversible acylation - Occurs when the acylation (covalent drug binding) is not
truly irreversible -- original target can be restored over time
Non-covalent bonds - Weaker bonds. Most common in drugs.
Functional groups must be close enough to interact (should have exposed sites)
Ionic Bond - Strongest type of non-covalent bond
Involves ionizable acidic (-) and basic (+)/ quat ammonium functional group
